886762-70-5Relevant articles and documents
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing
Furet, Pascal,Gerspacher, Marc,Pissot-Soldermann, Carole
supporting information; scheme or table, p. 1858 - 1860 (2010/07/04)
JAK2 is a target of high interest in chronic myeloproliferative disorders drug research. Starting from a screening hit, two new JAK2 inhibitor chemotypes were designed by scaffold morphing. The prototype compounds of these new series showed nanomolar inhi
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors
Pissot-Soldermann, Carole,Gerspacher, Marc,Furet, Pascal,Gaul, Christoph,Holzer, Philipp,McCarthy, Clive,Radimerski, Thomas,Regnier, Catherine H.,Baffert, Fabienne,Drueckes, Peter,Tavares, Gisele A.,Vangrevelinghe, Eric,Blasco, Francesca,Ottaviani, Giorgio,Ossola, Flavio,Scesa, Julien,Reetz, Janitha
scheme or table, p. 2609 - 2613 (2010/07/05)
We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compounds from this series have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.
Synthesis of pyrrolnitrin and related halogenated phenylpyrroles
Morrison, Matthew D.,Hanthorn, Jason J.,Pratt, Derek A.
supporting information; experimental part, p. 1051 - 1054 (2009/07/18)
A general approach to halogenated arylpyrroles, including the antifungal natural product pyrrolnitrin, is described using newly synthesized halogenated pyrroles and 2,6-disubstituted nitrobenzenes or 2,6-disubstituted anilines.
Benzimidazolone and dihydroindolone derivatives and uses thereof
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Page/Page column 64-65, (2008/06/13)
Compounds of the formula I: or pharmaceutically acceptable salts thereof wherein m, n, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.